Tag: M.W=150-200

Adamiak, Lisa published the artcilePeptide Brush Polymers and Nanoparticles with Enzyme-Regulated Structure and Charge for Inducing or Evading Macrophage Cell Uptake, SDS of cas: 6249-56-5, the publication is ACS Nano (2017), 11(10), 9877-9888, database is CAplus and MEDLINE.

Cellular uptake by macrophages and ensuing clearance by the mononuclear phagocyte system stands as a significant biol. barrier for nanoparticle therapeutics. While there is a growing body of work investigating the design principles essential for imparting nanomaterials with long-circulating characteristics and macrophage evasion, there is still a widespread need for examining stimuli-responsive systems, particularly well-characterized soft materials, which differ in their physiochem. properties prior to and after an applied stimulus. In this work, we describe the synthesis and formulation of polymeric nanoparticles (NPs) and soluble homopolymers (Ps) encoded with multiple copies of a peptide substrate for proteases. We examined the macrophage cell uptake of these materials, which vary in their peptide charge and conjugation (via the N- or C-terminus). Following treatment with a model protease, thermolysin, the NPs and Ps undergo changes in their morphol. and charge. After proteolysis, zwitterionic NPs showed significant cellular uptake, with the C-terminus NP displaying higher internalization than its N-terminus analog. Enzyme-cleaved homopolymers generally avoided assembly and uptake, though at higher concentrations, enzyme-cleaved N-terminus homopolymers assembled into discrete cylindrical structures, whereas C-terminus homopolymers remained dispersed. Overall, these studies highlight that maintaining control over NP and polymer design parameters can lead to well-defined biol. responses.

ACS Nano published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C7H16ClNO2, SDS of cas: 6249-56-5.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kobelev, Aleksandr I. published the artcileFacile regiodivergent synthesis of spiro pyrrole-substituted pseudothiohydantoins and thiohydantoins via reaction of [e]-fused 1H-pyrrole-2,3-diones with thiourea, Application In Synthesis of 3696-23-9, the publication is Beilstein Journal of Organic Chemistry (2019), 2864-2871, database is CAplus and MEDLINE.

A highly divergent synthesis of regioisomeric thiohydantoins and pseudothiohydantoins spiro-fused to a pharmacol. valuable pyrrole-2-one fragment involving the reaction of [e]-fused 1H-pyrrole-2,3-diones with thioureas was developed. The obtained spiro pseudothiohydantoin derivatives were found to undergo a pseudothiohydantoin-thiohydantoin rearrangement. The reactions were shown to proceed under catalyst-free conditions in good yields, and the products were isolated without applying preparative chromatog. methods.

Beilstein Journal of Organic Chemistry published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Application In Synthesis of 3696-23-9.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Etlis, V. S. published the artcileChlorination of some alkene sulfides, Safety of 1,2-Bis(2-chloroethyl)disulfane, the publication is Zhurnal Obshchei Khimii (1965), 35(3), 475-9, database is CAplus.

Ethylene sulfide and dry Cl₂ in CCl₄ under ultraviolet light at -5-0° 45-50 min. gave only (ClCH₂CH₂S)₂, b_1.5 87-8°, n²⁰_D 1.5655, d₂₀ 1.3381. Propylene sulfide similarly gave (ClCH₂CHMeS)₂, b₅ 128-9°, 1.5402, 1.2563; thioepichlorohydrin in a similar reaction gave [(ClCH₂)₂CHS]₂, m. 69°. Ethylene sulfide treated under N atm. with 0.125 mole Me₃COCl under ultraviolet light at -15° to -10° gave a mixture of Me₃COSCH₂CH₂Cl, b_1.5 37-8°, 1.4698, 1.0560, (ClCH₂CH₂S)₂, and some Me₃CO₂SCH₂CH₂Cl, b₁ 58-60°, 1.4853, 1.1510. Similar reaction of propylene sulfide gave Me₃COSCHMeCH₂Cl, b₁ 34°, 1.4641, 1.0269, and some (ClCH₂CHMeS)₂.

Zhurnal Obshchei Khimii published new progress about 1002-41-1. 1002-41-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is 1,2-Bis(2-chloroethyl)disulfane, and the molecular formula is C4H8Cl2S2, Safety of 1,2-Bis(2-chloroethyl)disulfane.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kim, Minsoo published the artcileStructure activity relationship exploration of 5-hydroxy-2-(3-phenylpropyl)chromones as a unique 5-HT_2B receptor antagonist scaffold, Computed Properties of 620-20-2, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(21), 127511, database is CAplus and MEDLINE.

Antagonists for the serotonin receptor 2B (5-HT_2B) have clin. applications towards migraine, anxiety, irritable bowl syndrome, and MDMA abuse; however, few selective 5-HT_2B antagonists have been identified. Previous studies from these labs identified a natural product, 5-hydroxy-2-(2-phenylethyl)chromone (5-HPEC, 2) as the first non-nitrogenous ligand for the 5-HT_2B receptor. Studies on 5-HPEC optimization led to the identification of 5-hydroxy-2-(3-phenylpropyl)chromone (5-HPPC, 3), which showed a tenfold improvement in binding affinity over 2 at 5-HT_2B. This study aimed to further improve receptor pharmacol. of this unique scaffold. Guided by mol. modeling studies modifications at the C-3′ and C-4′ positions of 3 were made to probe their effects on ligand binding affinity and efficacy. Among the derivatives synthesized 5-hydroxy-2-(3-(3-cyanophenyl)propyl)chromone (5-HCPC, 3d) showed the most promise with a multifold improvement in binding affinity (pK_i = 7.1 ± 0.07) over 3 with retained antagonism.

Bioorganic & Medicinal Chemistry Letters published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Computed Properties of 620-20-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kim, Minsoo published the artcileStructure activity relationship exploration of 5-hydroxy-2-(3-phenylpropyl)chromones as a unique 5-HT_2B receptor antagonist scaffold, SDS of cas: 939-99-1, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(21), 127511, database is CAplus and MEDLINE.

Antagonists for the serotonin receptor 2B (5-HT_2B) have clin. applications towards migraine, anxiety, irritable bowl syndrome, and MDMA abuse; however, few selective 5-HT_2B antagonists have been identified. Previous studies from these labs identified a natural product, 5-hydroxy-2-(2-phenylethyl)chromone (5-HPEC, 2) as the first non-nitrogenous ligand for the 5-HT_2B receptor. Studies on 5-HPEC optimization led to the identification of 5-hydroxy-2-(3-phenylpropyl)chromone (5-HPPC, 3), which showed a tenfold improvement in binding affinity over 2 at 5-HT_2B. This study aimed to further improve receptor pharmacol. of this unique scaffold. Guided by mol. modeling studies modifications at the C-3′ and C-4′ positions of 3 were made to probe their effects on ligand binding affinity and efficacy. Among the derivatives synthesized 5-hydroxy-2-(3-(3-cyanophenyl)propyl)chromone (5-HCPC, 3d) showed the most promise with a multifold improvement in binding affinity (pK_i = 7.1 ± 0.07) over 3 with retained antagonism.

Bioorganic & Medicinal Chemistry Letters published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, SDS of cas: 939-99-1.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Ahmad, Imran published the artcileSyntheses of lipophilic chalcones and their conformationally restricted analogues as antitubercular agents, Recommanded Product: 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(5), 1322-1325, database is CAplus and MEDLINE.

Lipophilic chalcones and their conformationally restricted analogs were synthesized and evaluated for their antitubercular efficacy against Mycobacterium tuberculosis H37Rv strain. Compounds I, II, and III [R = CH₂CH₂-(piperidin-1-yl), CH₂CHMeCH₂NMe₂] were found to be active MIC at 60, 30, 3.5 and 7.5 μg-mL^-1. In vitro cytotoxicity of compounds I, II, III [R = CH₂CH₂-(piperidin-1-yl), CH₂CHMeCH₂NMe₂] and IV in non-cancerous human epithelial kidney cell line (HEK-293) showed that most active compound III [CH₂CH₂-(piperidin-1-yl)] was approx. 2.85 times selective towards tubercular vs. healthy cells whereas II was found to be 16 times selective.

Bioorganic & Medicinal Chemistry Letters published new progress about 4584-49-0. 4584-49-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Salt,Amine,Aliphatic hydrocarbon chain, name is 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, and the molecular formula is C5H13Cl2N, Recommanded Product: 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Blake, Steven published the artcileSalicylanilide Analog Minimizes Relapse of Clostridioides difficile Infection in Mice, Product Details of C6H3ClFNO2, the publication is Journal of Medicinal Chemistry (2020), 63(13), 6898-6908, database is CAplus and MEDLINE.

Clostridioides difficile infection (CDI) causes serious and sometimes fatal symptoms like diarrhea and pseudomembranous colitis. Although antibiotics for CDI exist, they are either expensive or cause recurrence of the infection due to their altering the colonic microbiota, which is necessary to suppress the infection. Here, we leverage a class of known membrane-targeting compounds that we previously showed to have broad inhibitory activity across multiple Clostridioides difficile strains while preserving the microbiome to develop an efficacious agent. A new series of salicylanilides was synthesized, and the most potent analog was selected through an in vitro inhibitory assay to evaluate its pharmacokinetic parameters and potency in a CDI mouse model. The results revealed reduced recurrence of CDI and diminished disturbance of the microbiota in mice compared to standard-of-care vancomycin, thus paving the way for novel therapy that can potentially target the cell membrane of C. difficile to minimize relapse in the recovering patient.

Journal of Medicinal Chemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Product Details of C6H3ClFNO2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Jitchati, R. published the artcileThree synthetic routes to a commercial N3 dye, Category: chlorides-buliding-blocks, the publication is International Journal of Applied Physics and Mathematics (2012), 2(2), 107-110, database is CAplus.

We present the synthesis and characterization of a com. standard ruthenium dye namely, N3, by cheap and easily prepared starting materials from three synthetic routes: the Gratzel’s protocol and the other two new methods designed in our laboratory, i.e., the one-pot reaction and via the reaction of cymene complex.

International Journal of Applied Physics and Mathematics published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Category: chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Barnash, Kimberly D. published the artcileDiscovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2, Computed Properties of 6313-54-8, the publication is ACS Combinatorial Science (2017), 19(3), 161-172, database is CAplus and MEDLINE.

The function of EED within Polycomb repressive complex 2 (PRC2) is mediated by a complex network of protein-protein interactions. Allosteric activation of PRC2 by binding of methylated proteins to EED’s aromatic cage is essential for full catalytic activity, but details of this regulation are not fully understood. EED’s recognition of the product of PRC2 activity, histone H3 lysine 27 trimethylation (H3K27me3), stimulates PRC2 methyltransferase activity at adjacent nucleosomes leading to H3K27me3 propagation and, ultimately, gene repression. By coupling combinatorial chem. and structure-based design, we optimized a low affinity methylated Jarid2 peptide to a smaller, more potent peptidomimetic ligand (Kd = 1.14 ± 0.14 μM) of the aromatic cage of EED. Our strategy illustrates the effectiveness of applying combinatorial chem. to achieve both ligand potency and property optimization. Furthermore, the resulting ligands, UNC5114 and UNC5115, demonstrate that targeted disruption of EED’s reader function can lead to allosteric inhibition of PRC2 catalytic activity.

ACS Combinatorial Science published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Computed Properties of 6313-54-8.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Rajanarendar, E. published the artcileA Convenient and Facile Hantzsch Synthesis of Aryl Imidazo[1,2-b]Isoxazolyl-N-aryl Thiazol Amines, Quality Control of 3696-23-9, the publication is Journal of Heterocyclic Chemistry (2016), 53(6), 1983-1989, database is CAplus.

The Hantzsch synthesis of novel imidazo[1,2-b]isoxazolyl-N-arylthiazolamines analogs were described. Reaction of 3-amino-5-methylisoxazole with substituted phenacyl bromides in dry ethanol afforded the corresponding 6-methyl-3-arylimidazo[1,2-b]isoxazoles in good yields. The latter compounds on reaction with chloroacetyl chloride in 1,4-dioxane furnished the corresponding 2-chloro-1-(6-methyl-3-arylimidazo[1,2-b]isoxazol-2-yl)ethanones. These compounds on heating with N-arylthioureas in an oil bath underwent cyclization to afford the title compounds viz., imidazo[1,2-b]isoxazolyl-N-arylthiazolamines in moderate to good yields by Hantzsch synthesis.

Journal of Heterocyclic Chemistry published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Quality Control of 3696-23-9.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics